Search Results - "van Zeeland, Mario"

Dioxo-triazines as a novel series of cathepsin K inhibitors by Rankovic, Zoran, Cai, Jiaqiang, Fradera, Xavier, Dempster, Maureen, Mistry, Ashvin, Mitchell, Ann, Long, Clive, Hamilton, Emma, King, Angela, Boucharens, Sylviane, Jamieson, Craig, Gillespie, Jonathan, Cumming, Iain, Uitdehaag, Joost, Zeeland, Mario van

“…A series of potent and selective dioxo-triazine inhibitors of cathepsin K was identified from HTS. A novel dioxo-triazine series of cathepsin K inhibitors was…”
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Structure-based lead identification of ATP-competitive MK2 inhibitors by Barf, Tjeerd, Kaptein, Allard, Wilde, Sander de, Heijden, Ruud van der, Someren, Richard van, Demont, Dennis, Schultz-Fademrecht, Carsten, Versteegh, Judith, Zeeland, Mario van, Seegers, Nicole, Kazemier, Bert, Kar, Bas van de, Hoek, Maaike van, Roos, Jeroen de, Klop, Henri, Smeets, Ruben, Hofstra, Claudia, Hornberg, Jorrit, Oubrie, Arthur

“…MK2 kinase is a promising drug discovery target for the treatment of inflammatory diseases. Here, we describe the discovery of novel MK2 inhibitors using X-ray…”
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Discovery of selective and orally available spiro-3-piperidyl ATP-competitive MK2 inhibitors by Kaptein, Allard, Oubrie, Arthur, Zwart, Edwin de, Hoogenboom, Niels, Wit, Joeri de, Kar, Bas van de, Hoek, Maaike van, Vogel, Gerard, Kimpe, Vera de, Schultz-Fademrecht, Carsten, Borsboom, Judith, Zeeland, Mario van, Versteegh, Judith, Kazemier, Bert, Roos, Jeroen de, Wijnands, Frank, Dulos, John, Jaeger, Martin, Leandro-Garcia, Paula, Barf, Tjeerd

“…The identification of a potent, selective, and orally available MK2 inhibitor series is described. The initial absence of oral bioavailability was successfully…”
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Design and optimization of a series of novel 2-cyano-pyrimidines as cathepsin K inhibitors by Rankovic, Zoran, Cai, Jiaqiang, Kerr, Jennifer, Fradera, Xavier, Robinson, John, Mistry, Ashvin, Hamilton, Emma, McGarry, George, Andrews, Fiona, Caulfield, Wilson, Cumming, Iain, Dempster, Maureen, Waller, John, Scullion, Paul, Martin, Iain, Mitchell, Ann, Long, Clive, Baugh, Mark, Westwood, Paul, Kinghorn, Emma, Bruin, John, Hamilton, William, Uitdehaag, Joost, Zeeland, Mario van, Potin, Dominique, Saniere, Laurent, Fouquet, Andre, Chevallier, François, Deronzier, Hortense, Dorleans, Cecile, Nicolai, Eric

“…Morphing structural features of HTS-derived chemotypes led to the discovery of novel 2-cyano-pyrimidine inhibitors of cathepsin K with improved pharmacokinetic…”
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X-ray structure of p38α bound to TAK-715: comparison with three classic inhibitors by Azevedo, Rita, van Zeeland, Mario, Raaijmakers, Hans, Kazemier, Bert, de Vlieg, Jacob, Oubrie, Arthur

“…The p38α mitogen‐activated protein kinase regulates the synthesis of pro‐inflammatory cytokines in response to stimulation by a diverse set of stress signals…”
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X-ray structure of p38[alpha] bound to TAK-715: comparison with three classic inhibitors by Azevedo, Rita, van Zeeland, Mario, Raaijmakers, Hans, Kazemier, Bert, de Vlieg, Jacob, Oubrie, Arthur

“…The p38[alpha] mitogen-activated protein kinase regulates the synthesis of pro-inflammatory cytokines in response to stimulation by a diverse set of stress…”
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Trifluoromethylphenyl as P2 for ketoamide-based cathepsin S inhibitors by Cai, Jiaqiang, Robinson, John, Belshaw, Simone, Everett, Kathryn, Fradera, Xavier, van Zeeland, Mario, van Berkom, Leon, van Rijnsbergen, Peter, Popplestone, Lucy, Baugh, Mark, Dempster, Maureen, Bruin, John, Hamilton, William, Kinghorn, Emma, Westwood, Paul, Kerr, Jennifer, Rankovic, Zoran, Arbuckle, Wullie, Bennett, D. Jonathan, Jones, Philip S., Long, Clive, Martin, Iain, Uitdehaag, Joost C.M., Meulemans, Tommi

“…By using a small atom (Cl, F, or Me) to increase the torsion angle between the phenyl ring and the attached secondary amide, trifluoromethylphenyl motif was…”
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4-(3-Trifluoromethylphenyl)-pyrimidine-2-carbonitrile as cathepsin S inhibitors: N3, not N1 is critically important by Cai, Jiaqiang, Fradera, Xavier, van Zeeland, Mario, Dempster, Maureen, Cameron, Kenneth S., Bennett, D. Jonathan, Robinson, John, Popplestone, Lucy, Baugh, Mark, Westwood, Paul, Bruin, John, Hamilton, William, Kinghorn, Emma, Long, Clive, Uitdehaag, Joost C.M.

“…The N3 nitrogen of the pyrimidine-2-carbonitrile based cathepsin cysteine protease inhibitors is critically important. An ‘in situ double activation’ mechanism…”
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6-Phenyl-1H-imidazo[4,5-c]pyridine-4-carbonitrile as cathepsin S inhibitors by Cai, Jiaqiang, Baugh, Mark, Black, Darcey, Long, Clive, Jonathan Bennett, D., Dempster, Maureen, Fradera, Xavier, Gillespie, Jonathan, Andrews, Fiona, Boucharens, Sylviane, Bruin, John, Cameron, Kenneth S., Cumming, Iain, Hamilton, William, Jones, Philip S., Kaptein, Allard, Kinghorn, Emma, Maidment, Maurice, Martin, Iain, Mitchell, Ann, Rankovic, Zoran, Robinson, John, Scullion, Paul, Uitdehaag, Joost C.M., Vink, Paul, Westwood, Paul, van Zeeland, Mario, van Berkom, Leon, Bastiani, Martijn, Meulemans, Tommi

“…6-Phenyl-1H-imidazo[4,5-c]pyridine-4-carbonitrile derivatives were identified as selective human cathepsin S inhibitors with a stable thiol trapping nitrile…”
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2-Phenyl-9H-purine-6-carbonitrile derivatives as selective cathepsin S inhibitors by Cai, Jiaqiang, Bennett, D. Jonathan, Rankovic, Zoran, Dempster, Maureen, Fradera, Xavier, Gillespie, Jonathan, Cumming, Iain, Finlay, William, Baugh, Mark, Boucharens, Sylviane, Bruin, John, Cameron, Kenneth S., Hamilton, William, Kerr, Jennifer, Kinghorn, Emma, McGarry, George, Robinson, John, Scullion, Paul, Uitdehaag, Joost C.M., van Zeeland, Mario, Potin, Dominique, Saniere, Laurent, Fouquet, Andre, Chevallier, Francois, Deronzier, Hortense, Dorleans, Cecile, Nicolai, Eric

“…2-Phenyl-9H-purine-6-carbonitrile derivatives were designed as selective human cathepsin S inhibitors through P2 optimization and transition state…”
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Optimisation of 2-cyano-pyrimidine inhibitors of cathepsin K: Improving selectivity over hERG by Rankovic, Zoran, Cai, Jiaqiang, Kerr, Jennifer, Fradera, Xavier, Robinson, John, Mistry, Ashvin, Finlay, William, McGarry, George, Andrews, Fiona, Caulfield, Wilson, Cumming, Iain, Dempster, Maureen, Waller, John, Arbuckle, Wullie, Anderson, Mark, Martin, Iain, Mitchell, Ann, Long, Clive, Baugh, Mark, Westwood, Paul, Kinghorn, Emma, Jones, Phil, Uitdehaag, Joost C.M., van Zeeland, Mario, Potin, Dominique, Saniere, Laurent, Fouquet, Andre, Chevallier, François, Deronzier, Hortense, Dorleans, Cecile, Nicolai, Eric

“…Structure-guided optimisation strategies which led to a successful attenuation of hERG block in 2-cyano-pyrimidine series of catK inhibitors are described…”
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Capillary electrophoresis of peptides. Analysis of adrenocorticotropic hormone-related fragments by van de Goor, T A, Janssen, P S, van Nispen, J W, van Zeeland, M J, Everaerts, F M

“…Capillary electrophoresis can be used successfully to analyse small peptides to give additional information to that obtained using high-performance liquid…”
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